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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Wang Shouchuan, Huang Shaoling, Peng Feng, Wu Yanchun, Pan Weigao, Huang Yunhou, Luo Peng

Zhuang Medical College, Guangxi University of Chinese Medicine, Nanning, 530001, China.

Chem Biodivers. 2025 Feb;22(2):e202402016. doi: 10.1002/cbdv.202402016. Epub 2024 Nov 9.

The toxicity of derivatives was removed by the reasonable modification of bioactive skeleton. 2. As potential COX-2 inhibitor with IC values ranging from 39.42 to 179.84 nM/L, compounds (Q4-Q10, Q20) exhibited superior anti-inflammatory activity at low micromolar concentrations. 3. Q7 (IC= 61.05 nM/L), Q10 (IC= 54.68 nM/L) and Q20 (IC= 39.42 nM/L) showed stronger COX-2 inhibitory abilities than Celecoxib (IC= 67.89 nM/L). 4. The strongest anti-inflammatory agent, Q20 (IC= 9.96 μM/L, IC= 39.42 nM/L) effectively inhibited the secretion of IL-1β and TNF-α, exhibited the IC values of 12.30 and 9.07 μM/L respectively. 5. Q20 exerted as anti-inflammatory actives via targeting COX-2, down-regulating iNOS and TLR4 protein, and inhibiting the activation of NLRP3 inflammasome and NF-κB signal pathway.

通过对生物活性骨架进行合理修饰，去除了衍生物的毒性。2. 作为潜在的COX - 2抑制剂，化合物（Q4 - Q10，Q20）的IC值在39.42至179.84 nM/L之间，在低微摩尔浓度下表现出优异的抗炎活性。3. Q7（IC = 61.05 nM/L）、Q10（IC = 54.68 nM/L）和Q20（IC = 39.42 nM/L）显示出比塞来昔布（IC = 67.89 nM/L）更强的COX - 2抑制能力。4. 最强的抗炎剂Q20（IC = 9.96 μM/L，IC = 39.42 nM/L）有效抑制IL - 1β和TNF - α的分泌，其IC值分别为12.30和9.07 μM/L。5. Q20通过靶向COX - 2、下调iNOS和TLR4蛋白以及抑制NLRP3炎性小体和NF - κB信号通路的激活发挥抗炎活性。

Wang Shouchuan, Huang Shaoling, Peng Feng, Wu Yanchun, Pan Weigao, Huang Yunhou, Luo Peng

Zhuang Medical College, Guangxi University of Chinese Medicine, Nanning, 530001, China.

Chem Biodivers. 2025 Feb;22(2):e202402016. doi: 10.1002/cbdv.202402016. Epub 2024 Nov 9.

The toxicity of derivatives was removed by the reasonable modification of bioactive skeleton. 2. As potential COX-2 inhibitor with IC values ranging from 39.42 to 179.84 nM/L, compounds (Q4-Q10, Q20) exhibited superior anti-inflammatory activity at low micromolar concentrations. 3. Q7 (IC= 61.05 nM/L), Q10 (IC= 54.68 nM/L) and Q20 (IC= 39.42 nM/L) showed stronger COX-2 inhibitory abilities than Celecoxib (IC= 67.89 nM/L). 4. The strongest anti-inflammatory agent, Q20 (IC= 9.96 μM/L, IC= 39.42 nM/L) effectively inhibited the secretion of IL-1β and TNF-α, exhibited the IC values of 12.30 and 9.07 μM/L respectively. 5. Q20 exerted as anti-inflammatory actives via targeting COX-2, down-regulating iNOS and TLR4 protein, and inhibiting the activation of NLRP3 inflammasome and NF-κB signal pathway.

通过对生物活性骨架进行合理修饰，去除了衍生物的毒性。2. 作为潜在的COX - 2抑制剂，化合物（Q4 - Q10，Q20）的IC值在39.42至179.84 nM/L之间，在低微摩尔浓度下表现出优异的抗炎活性。3. Q7（IC = 61.05 nM/L）、Q10（IC = 54.68 nM/L）和Q20（IC = 39.42 nM/L）显示出比塞来昔布（IC = 67.89 nM/L）更强的COX - 2抑制能力。4. 最强的抗炎剂Q20（IC = 9.96 μM/L，IC = 39.42 nM/L）有效抑制IL - 1β和TNF - α的分泌，其IC值分别为12.30和9.07 μM/L。5. Q20通过靶向COX - 2、下调iNOS和TLR4蛋白以及抑制NLRP3炎性小体和NF - κB信号通路的激活发挥抗炎活性。